Self-Nanoemulsifying Drug Delivery Systems for Enhancing Solubility, Permeability, and Bioavailability of Sesamin.

Chih-Yuan Wang,Yu-Tse Wu,Ching-Chi Yen,Mei-Chich Hsu

doi:10.3390/molecules25143119

Abstract

Sesamin (SSM) is a water-insoluble compound that is easily eliminated by liver metabolism. To improve the solubility and bioavailability of SSM, this study developed and characterized a self-nanoemulsifying drug delivery system (SNEDDS) for the oral delivery of SSM and conducted pharmacokinetic assessments. Oil and surfactant materials suitable for SNEDDS preparation were selected on the basis of their saturation solubility at 37 ± 0.5 °C. The mixing ratios of excipients were determined on the basis of their dispersibility, transmittance (%), droplet sizes, and polydispersity index. An SNEDDS (F10) formulation comprising glyceryl trioctanoate, polyoxyethylene castor oil, and Tween 20 at a ratio of 10:10:80 (w/w/w) was the optimal formulation. This formulation maintained over 90% of its contents in different storage environments for 12 weeks. After the self-emulsification of SNEDDS, the SSM dispersed droplet size was 66.4 ± 31.4 nm, intestinal permeability increased by more than three-fold, relative bioavailability increased by approximately 12.9-fold, and absolute bioavailability increased from 0.3% to 4.4%. Accordingly, the developed SNEDDS formulation can preserve SSM’s solubility, permeability, and bioavailability. Therefore, this SNEDDS formulation has great potential for the oral administration of SSM, which can enhance its pharmacological application value.

Highlights

Sesame (Sesamum indicum L.) is part of the Pedaliaceae family, and it is planted in areas ranging from tropical to temperate zones in Africa, Asia, and Latin America
After 12 weeks of storage, the content of SSM–self-nanoemulsifying drug delivery system (SNEDDS) was. These results suggested that the encapsulation of SSM inof the may provide sufficient more. These results suggested that the encapsulation in the SNEDDS
The results indicated that this solid dispersion formulation provided a Cmax of 793 ng/mL, the time to maximum concentration (Tmax ) of 8 h, and a 30-fold improvement of the oral bioavailability of SSM when compared with that of the crystalline one

Summary

Introduction

Sesame (Sesamum indicum L.) is part of the Pedaliaceae family, and it is planted in areas ranging from tropical to temperate zones in Africa, Asia, and Latin America. The history of sesame consumption can be traced back to Assyria and Babylon 4000 years ago [1]. Sesame has several nutritional and health benefits. Studies on senescence-accelerated mice have revealed that the levels of reactive carbonyl species (RCs) in the cerebral cortex and liver increase with age. Basal diet supplementation with sesame lignan for 10 months was reported to reduce the levels of RCs in mice. Research has revealed that sesame lignans suppress cognitive decline by reducing age-related RCs production in the brain [2]

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Results

Conclusion